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GPCR/G Protein GHSR TC-G-1008

TC-G-1008

Catalog No. T4648   CAS 1621175-65-2
Synonyms: GPR39-C3, GPR39-C3

TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).

TC-G-1008, CAS 1621175-65-2
Pack Size Availability Price/USD Quantity
2 mg In stock 67.00
5 mg In stock 103.00
10 mg In stock 177.00
25 mg In stock 377.00
50 mg In stock 659.00
1 mL * 10 mM (in DMSO) In stock 103.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
Targets&IC50 rat GPR39 : ic50 0.4 nM,   human GPR39 : ic50 0.8 nM,  
Kinase Assay HEK293-GPR39 cells are plated and cultured in poly-d-lysine-coated, white, 384-well plates (4000 cells/well) in the growth medium overnight at 37°C in the presence of 5% CO2. For pretreatment of the cells with GPR39 ligands (TCG-1008) or vehicle control (DMSO), the culture medium is removed and the cells are stimulated with GPR39 ligands in assay buffer for the indicated time at 37°C. Then, the compound solution is removed and washed twice with PBS containing 0.1% BSA. For measurement of intracellular cAMP, the cells are stimulated with drugs in stimulation buffer for 30 min at 37°C. The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit[2] .
Animal Research
Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1] .
Synonyms GPR39-C3 , GPR39-C3
Purity 99.00%
Molecular Weight 418.9
Formula C18H19ClN6O2S
CAS No. 1621175-65-2

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 100 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Peukert S, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8. 2. Shimizu Y, et al. Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation. Biochem Pharmacol. 2017 Sep 15;140:105-114.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library

Related Products

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Anamorelin JMV 2959 hydrochloride TC-G-1008 Pralmorelin Pralmorelin acetate 158861-67-7(free base) Ibutamoren Mesylate AnaMorelin hydrochloride GHRP-6 acetate

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